2001
Novel Approaches to Polynuclear Platinum Pro-Drugs. Selective Release of Cytotoxic Platinum−Spermidine Species through Hydrolytic Cleavage of Carbamates
Hegmans A, Qu Y, Kelland L, Roberts J, Farrell N. Novel Approaches to Polynuclear Platinum Pro-Drugs. Selective Release of Cytotoxic Platinum−Spermidine Species through Hydrolytic Cleavage of Carbamates. Inorganic Chemistry 2001, 40: 6108-6114. PMID: 11703107, DOI: 10.1021/ic010509a.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAntineoplastic AgentsCarbamatesCatalysisChromatography, High Pressure LiquidFemaleHumansHydrogen-Ion ConcentrationHydrolysisInhibitory Concentration 50Leukemia L1210MiceMolecular StructureNuclear Magnetic Resonance, BiomolecularOrganoplatinum CompoundsOvarian NeoplasmsPolyaminesProdrugsSpermidineSpermineStereoisomerismStructure-Activity RelationshipTemperatureTumor Cells, CulturedConceptsDinuclear platinum compoundsPt–Cl bondsPreliminary biological assaysN-butyl side chainsMagnitude less cytotoxicPolynuclear platinumSecond generation analogsNMR spectroscopyPolyamine linkersQuaternary nitrogenFMOC derivativesConformational isomersDerivatives 4Electrostatic contributionSide chainsHydrolytic cleavageSpermidine moietyGreater selectivityOral deliveryTherapeutic indexPlatinum drugsRate constantsCellular uptakeN-propylBiological assays
1984
Efficacy and toxicity of 4-(2-sulfonatoethylthio)-cyclophosphamide cyclohexylamine salt (ASTA Z 7557, INN mafosfamide) after intraperitoneal administration to mice
Roberts J, Hacker M, Newman R, McCormack J, Krakoff I. Efficacy and toxicity of 4-(2-sulfonatoethylthio)-cyclophosphamide cyclohexylamine salt (ASTA Z 7557, INN mafosfamide) after intraperitoneal administration to mice. Investigational New Drugs 1984, 2: 215-220. PMID: 6469517, DOI: 10.1007/bf00232354.Peer-Reviewed Original ResearchConceptsBladder toxicityIntraperitoneal administrationAcute bladder toxicityPhosphoramide mustardAZ therapyHepatic fibrosisIntravenous administrationLocal toxicityTherapeutic indexMurine systemAdministrationCyclophosphamide analoguesFurther studiesSpontaneous activationAssociated riskToxicityCyclohexylamine saltFibrosisTherapyMice